The present paper describes the reduction of 1-methyl-5-nitro-benzimidazoles (1A, 2A) and 1,3-dimethyl-2H-5-nitro-benzimidazol-2-one (3) to 5-aminobenzimidazoles (4A, 5A) and 1,3-dimethyl-2H-5-amino-benzimidazol-2-one (6) respectively with hydrazine hydrate in absolute ethanol in the presence of graphite. Compounds 5A and 6 were converted to 2-ethyl-5-(phthaloyl-L-phenylalanyl)amino-1-methylbenzimidazole (7) and 1,3-dimethyl-5-(phthaloyl-L-phenylalanyl)aminobenzimidazol-2-one (8). Characterization of the synthesized compounds was done with the help of mass spectrometry and H-1 NMR spectroscopic studies. Optical activity of the amino acid derivatives 7 and 8 was also recorded.